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International Union of Basic and Clinical Pharmacology. CVIII. Calcium-Sensing Receptor Nomenclature, Pharmacology, and Function.

Katie Leach, Fadil M Hannan, Tracy M Josephs, Andrew N Keller, Thor C Møller, Donald T Ward, Enikö Kallay, Rebecca S Mason, Rajesh V Thakker, Daniela Riccardi, Arthur D Conigrave, Hans Bräuner-Osborne,

The calcium-sensing receptor (CaSR) is a class C G protein-coupled receptor that responds to multiple endogenous agonists and allosteric modulators, including divalent and trivalent cations, L-amino acids, γ-glutamyl peptides, polyamines, polycationic peptides, and protons. The CaSR plays a critical role in extracellular calcium (Ca2+ o) homeostasis, as demonstrated by the ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(3):558-604]

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Drug Resistance in Epilepsy: Clinical Impact, Potential Mechanisms, and New Innovative Treatment Options.

Wolfgang Löscher, Heidrun Potschka, Sanjay M Sisodiya, Annamaria Vezzani,

Epilepsy is a chronic neurologic disorder that affects over 70 million people worldwide. Despite the availability of over 20 antiseizure drugs (ASDs) for symptomatic treatment of epileptic seizures, about one-third of patients with epilepsy have seizures refractory to pharmacotherapy. Patients with such drug-resistant epilepsy (DRE) have increased risks of premature ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(3):606-638]

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Using Pharmacology to Squeeze the Life Out of Childhood Leukemia, and Potential Strategies to Achieve Breakthroughs in Medulloblastoma Treatment.

Juwina Wijaya, Tomoka Gose, John D Schuetz,

Eliminating cancer was once thought of as a war. This analogy is still apt today; however, we now realize that cancer is a much more formidable enemy than scientists originally perceived, and in some cases, it harbors a profound ability to thwart our best efforts to defeat it. However, before ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(3):668-691]

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Correction to "Targeting Janus Kinases and Signal Transducer and Activator of Transcription 3 to Treat Inflammation, Fibrosis, and Cancer: Rationale, Progress, and Caution".

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(3):605]

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The Noncanonical Pathway for In Vivo Nitric Oxide Generation: The Nitrate-Nitrite-Nitric Oxide Pathway.

V Kapil, R S Khambata, D A Jones, K Rathod, C Primus, G Massimo, J M Fukuto, A Ahluwalia,

In contrast to nitric oxide, which has well established and important roles in the regulation of blood flow and thrombosis, neurotransmission, the normal functioning of the genitourinary system, and the inflammation response and host defense, its oxidized metabolites nitrite and nitrate have, until recently, been considered to be relatively inactive. ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(3):692-766]

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Strategies to Modulate MicroRNA Functions for the Treatment of Cancer or Organ Injury.

Tae Jin Lee, Xiaoyi Yuan, Keith Kerr, Ji Young Yoo, Dong H Kim, Balveen Kaur, Holger K Eltzschig,

Cancer and organ injury-such as that occurring in the perioperative period, including acute lung injury, myocardial infarction, and acute gut injury-are among the leading causes of death in the United States and impose a significant impact on quality of life. MicroRNAs (miRNAs) have been studied extensively during the last two ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(3):639-667]

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More than Smoke and Patches: The Quest for Pharmacotherapies to Treat Tobacco Use Disorder.

M J Moerke, L R McMahon, J L Wilkerson,

Tobacco use is a persistent public health issue. It kills up to half its users and is the cause of nearly 90% of all lung cancers. The main psychoactive component of tobacco is nicotine, primarily responsible for its abuse-related effects. Accordingly, most pharmacotherapies for smoking cessation target nicotinic acetylcholine receptors ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(2):527-557]

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Monocarboxylate Transporters (SLC16): Function, Regulation, and Role in Health and Disease.

Melanie A Felmlee, Robert S Jones, Vivian Rodriguez-Cruz, Kristin E Follman, Marilyn E Morris,

The solute carrier family 16 (SLC16) is comprised of 14 members of the monocarboxylate transporter (MCT) family that play an essential role in the transport of important cell nutrients and for cellular metabolism and pH regulation. MCTs 1-4 have been extensively studied and are involved in the proton-dependent transport of ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(2):466-485]

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Transitioning from Basic toward Systems Pharmacodynamic Models: Lessons from Corticosteroids.

Vivaswath S Ayyar, William J Jusko,

Technology in bioanalysis, -omics, and computation have evolved over the past half century to allow for comprehensive assessments of the molecular to whole body pharmacology of diverse corticosteroids. Such studies have advanced pharmacokinetic and pharmacodynamic (PK/PD) concepts and models that often generalize across various classes of drugs. These models encompass ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(2):414-438]

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Encoding, Consolidation, and Renormalization in Depression: Synaptic Homeostasis, Plasticity, and Sleep Integrate Rapid Antidepressant Effects.

Tomi Rantamäki, Samuel Kohtala,

Recent studies have strived to find an association between rapid antidepressant effects and a specific subset of pharmacological targets and molecular pathways. Here, we propose a broader hypothesis of encoding, consolidation, and renormalization in depression (ENCORE-D), which suggests that, fundamentally, rapid and sustained antidepressant effects rely on intrinsic homeostatic mechanisms ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(2):439-465]

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Patient and Disease-Specific Induced Pluripotent Stem Cells for Discovery of Personalized Cardiovascular Drugs and Therapeutics.

David T Paik, Mark Chandy, Joseph C Wu,

Human induced pluripotent stem cells (iPSCs) have emerged as an effective platform for regenerative therapy, disease modeling, and drug discovery. iPSCs allow for the production of limitless supply of patient-specific somatic cells that enable advancement in cardiovascular precision medicine. Over the past decade, researchers have developed protocols to differentiate iPSCs ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(1):320-342]

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Pharmacology and Therapeutics of Bronchodilators Revisited.

M G Matera, C P Page, L Calzetta, P Rogliani, M Cazzola,

Bronchodilators remain the cornerstone of the treatment of airway disorders such as asthma and chronic obstructive pulmonary disease (COPD). There is therefore considerable interest in understanding how to optimize the use of our existing classes of bronchodilator and in identifying novel classes of bronchodilator drugs. However, new classes of bronchodilator ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(1):218-252]

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High-dimensionality Data Analysis of Pharmacological Systems Associated with Complex Diseases.

Jhana O Hendrickx, Jaana van Gastel, Hanne Leysen, Bronwen Martin, Stuart Maudsley,

It is widely accepted that molecular reductionist views of highly complex human physiologic activity, e.g., the aging process, as well as therapeutic drug efficacy are largely oversimplifications. Currently some of the most effective appreciation of biologic disease and drug response complexity is achieved using high-dimensionality (H-D) data streams from transcriptomic, ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(1):191-217]

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Imidazoline Receptor System: The Past, the Present, and the Future.

Pascal Bousquet, Alan Hudson, Jesús A García-Sevilla, Jun-Xu Li,

Imidazoline receptors historically referred to a family of nonadrenergic binding sites that recognize compounds with an imidazoline moiety, although this has proven to be an oversimplification. For example, none of the proposed endogenous ligands for imidazoline receptors contain an imidazoline moiety but they are diverse in their chemical structure. Three ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(1):50-79]

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The Psychopharmacology of Obsessive-Compulsive Disorder: A Preclinical Roadmap.

Henry Szechtman, Brian H Harvey, Erik Z Woody, Kurt Leroy Hoffman,

This review evaluates current knowledge about obsessive-compulsive disorder (OCD), with the goal of providing a roadmap for future directions in research on the psychopharmacology of the disorder. It first addresses issues in the description and diagnosis of OCD, including the structure, measurement, and appropriate description of the disorder and issues ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(1):80-151]

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G Protein-Coupled Receptors in Asthma Therapy: Pharmacology and Drug Action.

Stacy Gelhaus Wendell, Hao Fan, Cheng Zhang,

Asthma is a heterogeneous inflammatory disease of the airways that is associated with airway hyperresponsiveness and airflow limitation. Although asthma was once simply categorized as atopic or nonatopic, emerging analyses over the last few decades have revealed a variety of asthma endotypes that are attributed to numerous pathophysiological mechanisms. The ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(1):1-49]

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Solute Carrier Transporters as Potential Targets for the Treatment of Metabolic Disease.

Tina Schumann, Jörg König, Christine Henke, Diana M Willmes, Stefan R Bornstein, Jens Jordan, Martin F Fromm, Andreas L Birkenfeld,

The solute carrier (SLC) superfamily comprises more than 400 transport proteins mediating the influx and efflux of substances such as ions, nucleotides, and sugars across biological membranes. Over 80 SLC transporters have been linked to human diseases, including obesity and type 2 diabetes (T2D). This observation highlights the importance of ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(1):343-379]

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Organic Cation Transporters in Health and Disease.

Hermann Koepsell,

The organic cation transporters (OCTs) OCT1, OCT2, OCT3, novel OCT (OCTN)1, OCTN2, multidrug and toxin exclusion (MATE)1, and MATE kidney-specific 2 are polyspecific transporters exhibiting broadly overlapping substrate selectivities. They transport organic cations, zwitterions, and some uncharged compounds and operate as facilitated diffusion systems and/or antiporters. OCTs are critically involved ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2020, 72(1):253-319]

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Challenges and Opportunities for Childhood Cancer Drug Development.

Peter J Houghton, Raushan T Kurmasheva,

Cancer in children is rare with approximately 15,700 new cases diagnosed in the United States annually. Through use of multimodality therapy (surgery, radiation therapy, and aggressive chemotherapy), 70% of patients will be "cured" of their disease, and 5-year event-free survival exceeds 80%. However, for patients surviving their malignancy, therapy-related long-term ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2019, 71(4):671-697]

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International Union of Basic and Clinical Pharmacology. CVII. Structure and Pharmacology of the Apelin Receptor with a Recommendation that Elabela/Toddler Is a Second Endogenous Peptide Ligand.

Cai Read, Duuamene Nyimanu, Thomas L Williams, David J Huggins, Petra Sulentic, Robyn G C Macrae, Peiran Yang, Robert C Glen, Janet J Maguire, Anthony P Davenport,

The predicted protein encoded by the APJ gene discovered in 1993 was originally classified as a class A G protein-coupled orphan receptor but was subsequently paired with a novel peptide ligand, apelin-36 in 1998. Substantial research identified a family of shorter peptides activating the apelin receptor, including apelin-17, apelin-13, and ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2019, 71(4):467-502]

Cited: 2 times

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Beyond the Ligand: Extracellular and Transcellular G Protein-Coupled Receptor Complexes in Physiology and Pharmacology.

Henry A Dunn, Cesare Orlandi, Kirill A Martemyanov,

G protein-coupled receptors (GPCRs) remain one of the most successful targets of U.S. Food and Drug Administration-approved drugs. GPCR research has predominantly focused on the characterization of the intracellular interactome's contribution to GPCR function and pharmacology. However, emerging evidence uncovers a new dimension in the biology of GPCRs involving their ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2019, 71(4):503-519]

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Role of Voltage-Gated Sodium Channels in the Mechanism of Ether-Induced Unconsciousness.

Nicholas Denomme, Jacob M Hull, George A Mashour,

Despite continuous clinical use for more than 170 years, the mechanism of general anesthetics has not been completely characterized. In this review, we focus on the role of voltage-gated sodium channels in the sedative-hypnotic actions of halogenated ethers, describing the history of anesthetic mechanisms research, the basic neurobiology and pharmacology ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2019, 71(4):450-466]

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Targeting Foam Cell Formation in Atherosclerosis: Therapeutic Potential of Natural Products.

Dongdong Wang, Yang Yang, Yingnan Lei, Nikolay T Tzvetkov, Xingde Liu, Andy Wai Kan Yeung, Suowen Xu, Atanas G Atanasov,

Foam cell formation and further accumulation in the subendothelial space of the vascular wall is a hallmark of atherosclerotic lesions. Targeting foam cell formation in the atherosclerotic lesions can be a promising approach to treat and prevent atherosclerosis. The formation of foam cells is determined by the balanced effects of ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2019, 71(4):596-670]

Cited: 1 time

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Novel Therapeutic Approaches Targeting the Renin-Angiotensin System and Associated Peptides in Hypertension and Heart Failure.

Lauren B Arendse, A H Jan Danser, Marko Poglitsch, Rhian M Touyz, John C Burnett, Catherine Llorens-Cortes, Mario R Ehlers, Edward D Sturrock,

Despite the success of renin-angiotensin system (RAS) blockade by angiotensin-converting enzyme (ACE) inhibitors and angiotensin II type 1 receptor (AT1R) blockers, current therapies for hypertension and related cardiovascular diseases are still inadequate. Identification of additional components of the RAS and associated vasoactive pathways, as well as new structural and functional ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2019, 71(4):539-570]

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Druggable Transcriptional Networks in the Human Neurogenic Epigenome.

Gerald A Higgins, Aaron M Williams, Alex S Ade, Hasan B Alam, Brian D Athey,

Chromosome conformation capture methods have revealed the dynamics of genome architecture which is spatially organized into topologically associated domains, with gene regulation mediated by enhancer-promoter pairs in chromatin space. New evidence shows that endogenous hormones and several xenobiotics act within circumscribed topological domains of the spatial genome, impacting subsets of ... Read more >>

Pharmacol. Rev. (Pharmacological reviews)
[2019, 71(4):520-538]

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